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Related Concept Videos

Epigenetic Regulation01:37

Epigenetic Regulation

2.9K
Epigenetic changes alter the physical structure of the DNA without changing the genetic sequence and often regulate whether genes are turned on or off. This regulation ensures that each cell produces only proteins necessary for its function. For example, proteins that promote bone growth are not produced in muscle cells. Epigenetic mechanisms play an essential role in healthy development. Conversely, precisely regulated epigenetic mechanisms are disrupted in diseases like cancer.
X-chromosome...
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Spreading of Chromatin Modifications02:25

Spreading of Chromatin Modifications

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The histone proteins in the nucleosomes are post-translationally modified (PTM) to increase or decrease access to DNA. The commonly observed PTMs are methylation, acetylation, phosphorylation, and ubiquitination of lysine amino acids in the histone H3 tail region. These histone modifications have specific meaning for the cell. Hence, they are called "histone code". The protein complex involved in histone modification is termed as "reader-writer" complex.
Writers
The writer...
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Genomic DNA in Eukaryotes00:58

Genomic DNA in Eukaryotes

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Eukaryotes have large genomes compared to prokaryotes. To fit their genomes into a cell, eukaryotic DNA is packaged extraordinarily tightly inside the nucleus. To achieve this, DNA is tightly wound around proteins called histones, which are packaged into nucleosomes that are joined by linker DNA and coil into chromatin fibers. Additional fibrous proteins further compact the chromatin, which is recognizable as chromosomes during certain phases of cell division.
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Chromatin Immunoprecipitation- ChIP02:36

Chromatin Immunoprecipitation- ChIP

10.8K
Chromatin immunoprecipitation, or ChIP, is an antibody-based technique used to identify sites on DNA that bind to transcription factors of interest or histone proteins. It also helps determine the type of histone modifications such as acetylation, phosphorylation, or methylation.
Types of ChIP
ChIP can be divided into two types - X-ChIP and N-ChIP. X-ChIP involves in vivo cross-linking of histones and regulatory proteins to DNA, fragmenting the DNA by sonication, and isolating the protein-DNA...
10.8K
Histone Modification02:32

Histone Modification

12.8K
The histone proteins have a flexible N-terminal tail extending out from the nucleosome. These histone tails are often subjected to post-translational modifications such as acetylation, methylation, phosphorylation, and ubiquitination. Particular combinations of these modifications form “histone codes” that influence the chromatin folding and tissue-specific gene expression.
Acetylation
The enzyme histone acetyltransferase adds acetyl group to the histones. Another enzyme, histone...
12.8K
Eukaryotic Transcription Inhibitors01:52

Eukaryotic Transcription Inhibitors

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Certain biochemical processes, such as embryonic development and cell growth regulation, depend on the repression of specific genes. DNA binding proteins known as eukaryotic transcription inhibitors regulate the repression of gene expression in eukaryotes. The presence of these inhibitors at the required location and time in the cell is triggered by the presence of hormones and additional signals from other cells.
Eukaryotic transcription inhibitors usually contain two distinct domains, a...
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Related Experiment Video

Updated: May 9, 2025

Repressing Gene Transcription by Redirecting Cellular Machinery with Chemical Epigenetic Modifiers
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Repressing Gene Transcription by Redirecting Cellular Machinery with Chemical Epigenetic Modifiers

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Epigenetic reader chromodomain as a potential therapeutic target.

Shivangi Sharma1, J Trae Hampton1, Tatiana G Kutateladze2

  • 1Texas A&M Drug Discovery Center and Department of Chemistry, Texas A&M University College Station TX 77843 USA wsliu2007@tamu.edu.

RSC Chemical Biology
|April 30, 2025
PubMed
Summary

Chromodomains are key epigenetic readers involved in gene regulation and disease. This review highlights their roles, potential as therapeutic targets, and strategies for developing selective inhibitors for diseases like cancer.

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A Method to Study de novo Formation of Chromatin Domains
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A Method to Study de novo Formation of Chromatin Domains
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Area of Science:

  • Epigenetics
  • Molecular Biology
  • Biochemistry

Background:

  • Epigenetic mechanisms rely on enzymes and 'reader' proteins that bind histone modifications.
  • Chromodomains are a family of reader proteins recognizing lysine methylation, crucial for transcriptional regulation and chromatin remodeling.
  • Dysfunctional chromodomains are linked to cancer, neurodegenerative disorders, and developmental abnormalities.

Purpose of the Study:

  • To review the biological and pathological roles of chromodomains.
  • To highlight chromodomains as potential prognostic biomarkers and therapeutic targets.
  • To discuss challenges and recent advances in developing selective chromodomain inhibitors.

Main Methods:

  • Literature review of biological and pathological activities of chromodomains.
  • Analysis of recent progress in chromodomain inhibitor development.
  • Description of strategies to overcome selectivity challenges in inhibitor design.

Main Results:

  • Chromodomains play critical roles in gene regulation and are implicated in various human diseases.
  • Significant progress has been made in developing chromodomain inhibitors.
  • Sequence similarity among chromodomains poses challenges for designing selective inhibitors.

Conclusions:

  • Chromodomains represent attractive therapeutic targets for diseases.
  • Targeting chromodomains shows promise for combating various human diseases.
  • Advanced strategies are emerging to develop selective chromodomain inhibitors, despite sequence similarity challenges.